Scandium Triflate-Catalyzed N -[ 18 F]Fluoroalkylation of Aryl- Or Heteroaryl-Amines with [ 18 F]Epifluorohydrin under Mild Conditions.
Masayuki FujinagaTakayuki OhkuboTomoteru YamasakiKatsushi KumataNobuki NengakiMing-Rong ZhangPublished in: Organic letters (2022)
The scandium triflate-catalyzed N -[ 18 F]fluoroalkylation of aryl- or heteroaryl-amines with [ 18 F]epifluorohydrin ([ 18 F] 2 ) was investigated. This reaction is mild and provides one-step access to N -[ 18 F]fluoroalkylated aryl- or heteroaryl-amines, which are used for positron emission tomography imaging. The use of 2,2,2-trifluoroethanol as a cosolvent improved the reaction efficiency. The use of ( S )- and ( R )-[ 18 F] 2 produced the corresponding enantiomeric N -[ 18 F]fluoroalkylated anilines.